2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Carboxylesterase (CES)

Carboxylesterase (CES)

Carboxylesterase; Carboxylic-ester Hydrolase

Cboxylesterases (CES) are serine hydrolases belonging to the superfamily of proteins with α/β hydrolase fold. Cboxylesterases are widely distributed in many tissues including liver, intestine, lung and kidney. Cboxylesterases catalyze the ester cleavage of a large number of structurally diverse ester- or amide-containing substrates into the corresponding alcohol and carboxylic acid. Actually, Cboxylesterases can hydrolyze ester, thioester, amide, and carbamate linkages in a wide variety of endo- and xenobiotic compounds, thus playing key roles in both endobiotic metabolism, and in activation and/or detoxification of xenobiotics. In humans, three Cboxylesterases have been identified, namely human carboxylesterase 1 (CES1), CES2, and CES3. Among them, CES1 and CES2 are two widely studied isoenzymes involved in xenobiotic metabolism. Cboxylesterases play an important role in the metabolism of various xenobiotics including ester drugs and environmental toxicants, and also participate in lipid homeostasis[1].

Carboxylesterase (CES) Isoform Specific Products:

Carboxylesterase (CES) Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-144809
    Pancreatic lipase/Carboxylesterase 1-IN-1
    		99.92%
    Pancreatic lipase/Carboxylesterase 1-IN-1 (Compound 39) is a potent dual inhibitor of pancreatic lipase (PL) and human carboxylesterase 1A (hCES1A) with IC50 values of 2.13 µM and 0.055  µM against PL and hCES1A.
    Pancreatic lipase/Carboxylesterase 1-IN-1
  • HY-142688
    Carboxylesterase-IN-2
    		Inhibitor 99.91%
    Carboxylesterase-IN-2 (compound 4u) is a potent inhibitor of Carboxylesterase Notum with an IC50 less than or equal to 10 nM. Notum is a negative regulator of Wnt signaling acting through the hydrolysis of a palmitoleoylate ester, which is required for Wnt activity. Carboxylesterase-IN-2 has the potential for the research of cancer disease.
    Carboxylesterase-IN-2
  • HY-N3921
    Gancaonin I
    Gancaonin I, an Isoflavone, exhibits moderate inhibition on human carboxylesterase 2 (hCES2A) with IC50 of 1.72 μM. Gancaonin I inhibits hCES2A-mediated fluorescein diacetate (FD) hydrolysis.
    Gancaonin I
  • HY-120253
    Spirotetramat
    		Inducer
    Spirotetramat (BY-108330) is an orally active Insecticide and lipid biosynthesis inhibitor. Spirotetramat regulates the activities of superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px), with short-term exposure increasing their activities and long-term exposure altering their activities. Spirotetramat induces the activity and mRNA expression of carboxylesterase (CarE). Spirotetramat induces oxidative stress and lipid peroxidation in tadpoles. Spirotetramat is toxic to amphibian tadpoles and exhibits sublethal/non-lethal toxicity to amphibians. Spirotetramat causes death in immature psyllids, aphids, scale insects, mealybugs, whiteflies and thrips, and shows a high lethal rate against Cacopsylla pyri nymphs. Spirotetramat reduces the fecundity of Aphis gossypii. Spirotetramat induces tolerance in the offspring of exposed Aphis gossypii, and acts on Myzus persicae, Bemisia tabaci and Tetranychus urticae.
    Spirotetramat
  • HY-155228
    LK-44
    hCES2A-IN-2 (Compound 44) is an orally active human carboxylesterase 2 (hCES2A) inhibitor (IC50: 5.02 μM). hCES2A-IN-2 improves Irinotecan (HY-16562)-induced delayed diarrhea.
    LK-44
  • HY-118041
    PMPMEase-IN-1
    		Inhibitor
    PMPMEase-IN-1 is an allylated methylated protein methylesterase inhibitor with the property of inhibiting PMPMEase activity. PMPMEase-IN-1 may provide a useful strategy for cancer inhibition by enhancing its affinity for polyisoprenyl derivatives. PMPMEase-IN-1 showed the potential to have an effective concentration (EC50) value in causing degeneration of human neuroblastoma SH-SY5Y cells. Specific inhibition of PMPMEase-IN-1 may help regulate the metabolism of polyisoprenyl proteins and thus maintain normal cell survival. Further development and application of PMPMEase-IN-1 may open up new avenues for inhibiting degenerative diseases and cancer.
    PMPMEase-IN-1
  • HY-147331
    Oseltamivir acid methyl ester
    		Inhibitor
    Oseltamivir acid methyl ester is a precursor form of the neuraminidase inhibitor and antiviral oseltamivir acid. Oseltamivir acid methyl ester is converted to oseltamivir acid by carboxylesterase 1 (CES1).
    Oseltamivir acid methyl ester
  • HY-147915
    Benz-AP
    		Inhibitor
    Benz-AP is a potent photosensitizer. Benz-AP produces singlet oxygen, with a negative correlation with hCES2 (Human carboxylesterase 2) activity. Benz-AP displays a higher photocytotoxicity potency in cancer cells under low hCES2 environments. Upon TPE (Two-photon excitation), Benz-AP produces ROS and kills cancer cells and tumor spheroids.
    Benz-AP
  • HY-176465
    CES2A-IN-3
    		Inhibitor
    CES2A-IN-3 (Compound 9d) is a potent serine-targeting covalent human carboxylesterase 2A (hCES2A) inhibitor with an IC50 value of 0.12 nM. CES2A-IN-3 is promising for research of diarrhea and ulcerative colitis.
    CES2A-IN-3
  • HY-169068
    Antifeedant agent 1
    		Inhibitor
    Antifeedant agent 1 is a carboxylesterase inhibitor that exerts insecticidal activity by inhibiting insect feeding, with an EC50 value of 0.038 mg/mL. Antifeedant agent 1 can be used in research related to pest control.
    Antifeedant agent 1
  • HY-D1739
    DDAO phosphate diammonium
    DDAO phosphate diammonium is a fluorescent phosphatase substrate. DDAO phosphate diammonium has tunable excitation wavelength (600-650nm) and long emission wavelength (λem=656nm). DDAO phosphate diammonium can be used to detect the activity of different enzymes such as β-galactosidase, sulfatase, protein phosphatase 2A, carboxylesterase 2, human albumin and esterase.
    DDAO phosphate diammonium
  • HY-N3413
    Kushenol X
    Kushenol X, a flavonoid compound isolated from the roots of Sophora flavescens. Kushenol X is a potent β-glucuronidase and human carboxylesterase 2 (hCE2) inhibitor with IC50s of 2.07 μM and 3.05 μM, respectively.
    Kushenol X
  • HY-176840
    Carboxylesterase-IN-4
    		Inhibitor
    Carboxylesterase-IN-4 (compound 3e) is a potent carboxylesterase inhibitor with an IC50 of 1.58 nM. Carboxylesterase-IN-4 can be used in the study of cholesterolemia.
    Carboxylesterase-IN-4
  • HY-W701476
    Ethyl phenylglyoxylate-d5
    Ethyl phenylglyoxylate-d5 (Ethyl benzoylformate-d5; Phenylglyoxylic acid ethyl ester-d5) is the deuterium labeled Ethyl phenylglyoxylate (HY-W016618). Ethyl phenylglyoxylate (Ethyl benzoylformate), the ethyl ester of phenylglyoxylic acid, is used as a synthetic reagent. Ethyl phenylglyoxylate is also a poor substrate but a potent inhibitor of chicken liver carboxylesterase. Additionally, Ethyl phenylglyoxylate exhibits photoreactivity, where its excited triplet carbonyl can initiate intermolecular hydrogen abstraction, radical coupling and cross-linking reactions.
    Ethyl phenylglyoxylate-d<sub>5</sub>
  • HY-P4611
    Z-Pro-Ala
    Z-Pro-Ala is an acid carboxypeptidase. Z-Pro-Ala can be isolated from grains and leaves of wheat, Triticum aestivum L.
    Z-Pro-Ala
  • HY-176841
    Carboxylesterase-IN-5
    		Inhibitor
    Carboxylesterase-IN-5 (Compound 2e) is an irreversible and competitive Carboxylesterase (CES) inhibitor with an IC50 of 21.7  nM for porcine liver CES. Carboxylesterase-IN-5 can be used for hypocholesterolemia research.
    Carboxylesterase-IN-5
  • HY-N0235R
    Bakuchiol (Standard)
    		Inhibitor
    Bakuchiol (Standard) is the analytical standard of Bakuchiol. This product is intended for research and analytical applications. Bakuchiol is a phytoestrogen that can be obtained from psoralen seeds. Bakuchiol has been proven to be a non-competitive inhibitor of multiple enzymes, including UDP-glucuronosyltransferase 2B7 (UGT2B7) and human carboxylesterase 2 (hCE2) , with IC50s values of 40.9 μM and 7.28 μM, respectively. Bakuchiol exhibits significant research and application potential in areas such as anti-inflammatory, antibacterial, antitumor therapies, as well as drug metabolism regulation.
    Bakuchiol (Standard)
  • HY-N1377R
    Nevadensin (Standard)
    		Inhibitor
    Nevadensin (Standard) (Lysionotin (Standard)) is the analytical standard of Nevadensin (HY-N1377). This product is intended for research and analytical applications. Nevadensin, a natural flavonoid, is a selective human carboxylesterase 1 (hCE1) inhibitor with an IC50 of 2.64 μM. Nevadensin is more selective for hCE1 than hCE2 (IC50 of 132.8 μM). Nevadensin can induce apoptosis and DNA damage in cancer cells. Nevadensin has a variety of pharmacological effects such as anti-inflammatory, anti-tumour, anti-hypertensive, anti-tubercular, antitussive, antioxidant and anti-microbial activities.
    Nevadensin (Standard)
  • HY-147331A
    Oseltamivir acid methyl ester hydrochloride
    		Inhibitor
    Oseltamivir acid methyl ester hydrochloride is a precursor form of the neuraminidase inhibitor and antiviral oseltamivir acid. Oseltamivir acid methyl ester hydrochloride is converted to oseltamivir acid by carboxylesterase 1 (CES1).
    Oseltamivir acid methyl ester hydrochloride
  • HY-E70599
    Human CES2 Enzyme
    Human CES2 Enzyme is a carboxylesterase involved in drug metabolism and lipid homeostasis. Human CES2 Enzyme hydrolyzes triglycerides, cholesteryl esters and retinyl esters to regulate lipid metabolism and energy homeostasis. Human CES2 Enzyme improves glucose tolerance and insulin sensitivity, reduces hepatic lipid accumulation, alleviates white adipose tissue steatitis, decreases plasma cholesterol levels, and reduces body weight and white adipose tissue weight. Human CES2 Enzyme can be used in the research of metabolic syndrome.
    Human CES2 Enzyme
Carboxylesterase (CES) Isoform Comparison

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